Enalapril Izvarino pills 20mg N20
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Description
Enalapril Izvarino pills - an ACE inhibitor. It is a prodrug from which the active metabolite enalaprilat is formed in the body. The mechanism of antihypertensive action is believed to be associated with competitive inhibition of ACE activity, which leads to a decrease in the rate of angiotensin I conversion to angiotensin II (which has a pronounced vasoconstrictor effect and stimulates the secretion of aldosterone in the adrenal cortex). plasma by eliminating negative feedback during renin release and a direct decrease in aldosterone secretion. In addition, enalaprilat appears to have an effect on the kinin-kallikrein system, preventing the breakdown of bradykinin. Due to its vasodilating effect, it decreases OPSP (afterload), the jamming pressure in the pulmonary capillaries (preload) and resistance in the pulmonary vessels, increases the minute volume of the heart and load tolerance.
Active ingredients
Enalapril
Release form
Pills
Pharmacological effect
Enalapril is an antihypertensive agent whose mechanism of dysissvy is associated with the inhibition of the activity of the agiotensin-rotating enzyme (A11F), which leads to a decrease in the formation of angiotensin I. Enalaprilat is formed as a result of hydrolysis of enalapril, which inhibits ACE. The mechanism of action is associated with a decrease in the formation of angiotensin II from angiotensin I, a decrease in the concentration of which leads to a direct decrease in the secretion of aldosterone. At the same time, total peripheral vascular resistance, systolic and diastolic blood pressure (BP), post- and preload on the myocardium decrease. Enalapril dilates the arteries to a greater extent than the veins, while there is no reflex increase in heart rate. Reduces the degradation of bradykinin, increases the synthesis of prostaglandins. The antihypertensive effect is more pronounced with high renin activity than with its normal or reduced activity. Reducing blood pressure in therapeutic limits does not affect cerebral circulation. The blood flow in the vessels of the brain is maintained at a sufficient level and against the background of low blood pressure. Enhances coronary and renal blood flow.With prolonged use, enalapril reduces hypertrophy of the left ventricle of the myocardium and myocytes of the arterial walls of the resistive type, prevents the progression of chronic heart failure (CHF), slows down the development of left ventricular dilatation, improves the blood supply to the ischemic myocardium. It has some diuretic effect. Reduces the inside of glomerular hypertension, slowing the development of glomerulosclerosis and the risk of chronic renal failure (CRF). With prolonged use in patients with reduced glomerular filtration rate, it reduces the symptoms of fluid retention and sodium in the body, and also has a positive effect on the ratio of lipoprotein fractions. In addition, the use of enalapril is characterized by the absence of influence or a positive effect on the concentration of total cholesterol. The time of onset of the antihypertensive effect when administered orally is 1 hour, reaches a maximum after 4-6 hours and lasts up to 24 hours. Some patients need therapy for several weeks to achieve optimal blood pressure. With CHF, a noticeable clinical effect is observed with prolonged treatment - 6 months or more. The duration of therapeutic action is dose-dependent.
Pharmacokinetics
After ingestion, about 60% enalapril is absorbed. Food intake does not affect absorption. After absorption, enalapril is rapidly hydrolyzed to form the active metabolite enalaprilat, which is a more active ACE inhibitor than enalapril. The linkage of enalaprilat with plasma proteins is 50-60%. The maximum concentration of enalaprilat in the blood serum is observed after 3-4 hours, enalapril - after 1 hour. Stable serum concentrations - after 4 days. The degree of absorption and hydrolysis of enalapril is the same for different doses within the recommended therapeutic range. Enalaprilat easily penetrates histohematogenous barriers, excluding the blood-brain barrier, a small amount penetrates through the placenta and into breast milk. Enalaprilat is eliminated mainly by the kidneys - 60% (20% - in the form of enlapril and 40% - in the form of enalaprilat), through the intestine - 33% (6% - in the form of enalapril and 27% - in the form of enalaprilat).The main metabolites detected in the urine are enalaprilat, approximately 40% of the dose taken, and unchanged enalapril. Data on other metabolites of enalapril no. The plasma concentration profile of enalaprilat has a long end phase, apparently due to its binding to ACE. The elimination half-life of enalaprilat is about 11 hours. It is removed during hemodialysis (speed 62 ml / min) and peritoneal dialysis.
Indications
Arterial hypertension (including renovascular hypertension), chronic heart failure (as part of a combination therapy), prevention of the development of clinically significant heart failure in patients with asymptomatic left ventricular dysfunction (as part of a combination therapy).
Dosage and administration
Inside, washing down with a small amount of liquid. Tablets can be taken before. during or after meals, regularly and at the same time of day. If the drug enalapril missed, you should take the missed dose. If there are several hours before the next dose is taken, the missed dose of Enalapril should not be taken. The dose should never be doubled. If it is necessary to take the drug in a dosage of 2.5 mg, it is possible to use enalapril in pills of 2.5 mg or 'L pills in dosages of 5 mg (with the risk - if available). Arterial hypertension The initial dose is from 5 to 20 mg 1 time per day, depending on the severity of arterial hypertension. The maximum daily dose of -40 mg / day once or in 2 divided doses.